Anti-VEGF

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Anti-VEGF therapy refers to a treatment approach aimed at inhibiting the action of vascular endothelial growth factor (VEGF), a signal protein produced by cells that stimulates vasculogenesis and angiogenesis. VEGF is a critical factor in the process of blood vessel formation, and its overexpression is associated with various diseases, including several types of cancer, age-related macular degeneration (AMD), and diabetic retinopathy. By blocking VEGF, anti-VEGF therapies can slow or halt the growth of tumors by starving them of the necessary blood supply and can also reduce the abnormal blood vessel growth in the eye that leads to vision loss.

Mechanism of Action[edit | edit source]

Anti-VEGF drugs work by targeting the VEGF proteins or their receptors on the surface of cells. By binding to these proteins or receptors, the drugs prevent VEGF from interacting with its receptors on the surface of endothelial cells, which form the lining of blood vessels. This inhibition prevents the signal that would normally initiate new blood vessel formation from being received, thereby inhibiting the process of angiogenesis.

Applications[edit | edit source]

Cancer Treatment[edit | edit source]

In the context of cancer, tumors require a constant supply of nutrients and oxygen to grow and spread. They achieve this by secreting high levels of VEGF, stimulating the formation of new blood vessels around them, a process known as tumor angiogenesis. Anti-VEGF therapies, such as bevacizumab (Avastin), are used to treat various cancers, including colorectal, lung, breast, glioblastoma, kidney, and ovarian cancers, by inhibiting this process.

Ophthalmology[edit | edit source]

In ophthalmology, anti-VEGF medications, including ranibizumab (Lucentis), aflibercept (Eylea), and bevacizumab (used off-label), are used to treat conditions characterized by the growth of abnormal blood vessels in the eye, such as AMD and diabetic retinopathy. These drugs are administered via injection directly into the eye and work by reducing the growth of abnormal vessels and decreasing fluid leakage, which can lead to vision improvement or stabilization.

Types of Anti-VEGF Agents[edit | edit source]

There are several types of anti-VEGF agents, each with a different mechanism of action:

  • Monoclonal Antibodies: These are laboratory-produced molecules that can precisely target and bind to VEGF proteins, preventing them from activating VEGF receptors. Bevacizumab is an example of a monoclonal antibody.
  • Fusion Proteins: These are created by fusing parts of different proteins together. Aflibercept is a fusion protein that acts as a decoy receptor, binding VEGF and preventing it from activating its natural receptors.
  • Small Molecule Tyrosine Kinase Inhibitors: These drugs, such as sunitinib (Sutent) and sorafenib (Nexavar), inhibit the activity of multiple tyrosine kinases, including those involved in VEGF signaling, thereby blocking angiogenesis.

Side Effects[edit | edit source]

While anti-VEGF therapy is a powerful tool in treating various diseases, it can also lead to several side effects due to its mechanism of action. These can include hypertension, proteinuria, wound healing complications, and in rare cases, gastrointestinal perforation. In the context of eye injections, potential side effects include eye pain, floaters, and the risk of infection.

Conclusion[edit | edit source]

Anti-VEGF therapy represents a significant advancement in the treatment of diseases characterized by abnormal angiogenesis and vasculogenesis. By targeting the VEGF pathway, these therapies offer a means to control the progression of diseases such as cancer and AMD, improving patient outcomes. Ongoing research continues to expand the potential applications of anti-VEGF agents and to refine their use to maximize benefits and minimize risks.

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Contributors: Prab R. Tumpati, MD